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Novel P2X 7 receptor antagonists ease the pain
Author(s) -
King B F
Publication year - 2007
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0707266
Subject(s) - potency , receptor , pharmacology , pain relief , clinical pharmacology , medicine , neuroscience , psychology , chemistry , anesthesia , in vitro , biochemistry
In recent months, a series of chemically diverse antagonists has been identified for the ATP‐gated P2X 7 receptor. In particular, two classes of highly‐selective competitive P2X 7 antagonists have been developed by Michael Jarvis and his colleagues at Abbott Laboratories. These di‐substituted tetrazole and cyanoguanidine derivatives are outstanding for a number of reasons (not least their stability, selectivity, potency and, of course, reversibility); most exciting is their near equal potency at human and rodent P2X 7 isoforms. Armed with drugs such as A740003 and newer A438079, Jarvis and colleagues have explored the role of P2X 7 receptors in the onset and persistence of chronic pain in animal models. Their findings ‐ and applicability to the human condition ‐ are reviewed in this current issue of British Journal of Pharmacology . This accompanying Commentary describes the progress made by Jarvis and others in developing novel P2X 7 antagonists for pain relief. British Journal of Pharmacology (2007) 151 , 565–567; doi: 10.1038/sj.bjp.0707266